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Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2,...
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Assessment of μ-Opioid Receptor Signaling Responses for Fentanyl Analogs Using Luciferase Complementation Assay.

Yasushi Ono1, Kuniaki Tayama1, Kosho Makino2

  • 1Department of Pharmaceutical and Environmental Sciences, Tokyo Metropolitan Institute of Public Health, 3-24-1 Hyakunin-cho, Shinjuku-ku, Tokyo 169-0073, Japan.

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Summary

Fentanyl analogs were tested for liver and kidney toxicity. Researchers found that while some analogs activate μ-opioid receptor (MOR) signaling, their desphenethylated metabolites do not, suggesting a potential pathway for safer drug development.

Keywords:
HEK293 celldesphenethylated metabolitefentanyl analogμ-opioid receptor

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Area of Science:

  • Pharmacology
  • Toxicology
  • Neuroscience

Background:

  • Fentanyl analogs are potent synthetic opioids with significant abuse potential.
  • Hepatotoxicity and nephrotoxicity are serious concerns associated with opioid use.
  • Understanding μ-opioid receptor (MOR) signaling is crucial for developing safer analgesics.

Purpose of the Study:

  • To investigate the potential liver and kidney toxicity of fentanyl analogs.
  • To evaluate the μ-opioid receptor (MOR) signaling profiles of fentanyl analogs and their metabolites.

Main Methods:

  • HEK293 cells were used to examine two types of MOR signaling responses: Gi and β-arrestin 2 recruitment.
  • The 50% effective concentration (EC50) and maximum response (Emax) were determined for each analog.
  • Desphenethylated metabolites were also assessed for MOR signaling activity.

Main Results:

  • In the MOR-mini-Gi assay, iBF showed the lowest EC50 and highest Emax, indicating potent Gi signaling.
  • In the MOR-β-arrestin 2 assay, DAMGO exhibited the highest Emax, suggesting strong β-arrestin 2 recruitment.
  • Desphenethylated metabolites demonstrated no MOR signaling activity.

Conclusions:

  • Fentanyl analogs exhibit varying degrees of MOR signaling bias towards Gi or β-arrestin 2 pathways.
  • The lack of MOR signaling by desphenethylated metabolites suggests they may not contribute to opioid-related toxicity.
  • Further research into these analogs and their metabolites could inform the development of safer pain therapeutics.